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Chemical Compound Review

Setrovel     [(1S,5S)-8-methyl-8- azabicyclo[3.2.1]oct-3...

Synonyms: Navoban, Tropisteron, tropisetron, AG-J-86351, ICS-205930, ...
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Disease relevance of Tropisteron


Psychiatry related information on Tropisteron


High impact information on Tropisteron


Chemical compound and disease context of Tropisteron


Biological context of Tropisteron


Anatomical context of Tropisteron

  • Since T cells play a key role in the onset of several inflammatory diseases, we have evaluated the immunosuppressive activity of tropisetron in human T cells, discovering that this compound is a potent inhibitor of early and late events in TCR-mediated T cell activation [24].
  • Intracisternal administration of tropisetron decreased the orofacial nocifensive behavior in the late phase evoked by the injection of formalin into the masseter muscle [25].
  • 7 Tropisetron (10 microM), SDZ 205-557 (3 microM) and GR 113808 (10-100 nM) caused an increase in basal tone of the rat terminal ileum when administered in the presence of methysergide and atropine [26].
  • Injection of tropisetron (0.005 and 0.01 microgram) or ondansetron (1.0 and 2.5 micrograms) into the hippocampus increased punished consumption of water in the Vogel conflict test [7].
  • The 5-HT(3) receptor-specific antagonist tropisetron blocked only the mCPBG-induced responses, but not the nicotinic responses on the same synaptosomes [27].

Associations of Tropisteron with other chemical compounds


Gene context of Tropisteron

  • Enzyme kinetics for formation of 5-hydroxy (5-OH-ICS), 6-hydroxy (6-OH-ICS) and N-demethyl tropisetron (N-De-ICS) were studied in the microsomal fraction of eight human livers (seven livers from extensive metabolizer (EM), one liver from a poor metabolizer (PM) for CYP2D6) [22].
  • Because these are the major pathways in vivo, coadministration of drugs competing for CYP2D6 and possibly CYP3A4 could influence the human kinetics of tropisetron and ondansetron [33].
  • In conclusion, our data show that the binding of tropisetron to 5-HT3 receptors results in antiinflammatory effects through inhibition of TNF-alpha/IL-1beta, which might explain the antiphlogistic effects of 5-HT3 antagonists [34].
  • Furthermore, pretreatment with 5-HT2A receptor antagonist (ketanserin), but not with 5-HT3 receptor antagonist (tropisetron), attenuated the behavioral response after the injection of 5-HT [35].
  • In order to assess the effect of antagonizing 5-HT2A or 5-HT3 receptors on formalin-induced Fos-LI, rats were pre-treated with local (masseter muscle) administration of ketanserin or tropisetron (0.01, 0.1 mg/rat) 20 min prior to formalin injection [36].

Analytical, diagnostic and therapeutic context of Tropisteron

  • PATIENTS AND METHODS: One thousand seventy-two patients, who were scheduled to receive at least two identical cycles of emetogenic chemotherapy, were treated with 5 mg tropisetron once daily in their first chemotherapy course [37].
  • METHODS: Twenty-six rapid metabolizers of tropisetron were included in this double-blind crossover study [38].
  • Tropisetron seems to be a promising and well tolerated drug in conjunction with extended radiotherapy of abdominal fields [39].
  • In a multicentre trial, 78 patients with a variety of malignancies, who had experienced insufficient control of emesis (greater than or equal to 3 episodes within 24 hours) while receiving standard antiemetics during previous chemotherapy, were randomly assigned to receive tropisetron 5mg once daily for 5 days or conventional antiemetic drugs [1].
  • Effects of 5HT3 receptor antagonism by tropisetron on the sleep EEG and on nocturnal hormone secretion [31].


  1. Prevention of chemotherapy-induced nausea and emesis in patients responding poorly to previous antiemetic therapy. Comparing tropisetron with optimised standard antiemetic therapy. Bruntsch, U., Drechsler, S., Hiller, E., Eiermann, W., Tulusan, A.H., Bühner, M., Hartenstein, R., Koenig, H.J., Gallmeier, W.M. Drugs (1992) [Pubmed]
  2. Pharmacology, toxicology and human pharmacokinetics of tropisetron. Kutz, K. Ann. Oncol. (1993) [Pubmed]
  3. Treatment of diarrhea in carcinoid syndrome with ondansetron, tropisetron, and clonidine. Schwörer, H., Münke, H., Stöckmann, F., Ramadori, G. Am. J. Gastroenterol. (1995) [Pubmed]
  4. The prophylactic effect of tropisetron on epidural morphine-related nausea and vomiting: a comparison of dexamethasone with saline. Wang, J.J., Tzeng, J.I., Ho, S.T., Chen, J.Y., Chu, C.C., So, E.C. Anesth. Analg. (2002) [Pubmed]
  5. A randomized double-blind placebo-controlled study of tropisetron in the treatment of outpatients with generalized anxiety disorder. Lecrubier, Y., Puech, A.J., Azcona, A., Bailey, P.E., Lataste, X. Psychopharmacology (Berl.) (1993) [Pubmed]
  6. Contribution of the peripheral 5-HT 2A receptor to mechanical hyperalgesia in a rat model of neuropathic pain. Nitanda, A., Yasunami, N., Tokumo, K., Fujii, H., Hirai, T., Nishio, H. Neurochem. Int. (2005) [Pubmed]
  7. Serotonergic innervation of the hippocampus and nucleus accumbens septi and the anxiolytic-like action of the 5-HT3 receptor antagonists. Stefański, R., Pałejko, W., Bidziński, A., Kostowski, W., Płaźnik, A. Neuropharmacology (1993) [Pubmed]
  8. The pharmacology of the 5-HT4 receptor. Costall, B., Naylor, R.J. International clinical psychopharmacology. (1993) [Pubmed]
  9. Alcohol drinking in rats treated with 5,7-dihydroxytryptamine: effect of 8-OH-DPAT and tropisetron (ICS 205-930). Jankowska, E., Bidzinski, A., Kostowski, W. Alcohol (1994) [Pubmed]
  10. Adverse reaction to 5-HT3 antagonist ICS 205930. Coupe, M. Lancet (1987) [Pubmed]
  11. Patient-tailored antiemetic treatment with 5-hydroxytryptamine type 3 receptor antagonists according to cytochrome P-450 2D6 genotypes. Kaiser, R., Sezer, O., Papies, A., Bauer, S., Schelenz, C., Tremblay, P.B., Possinger, K., Roots, I., Brockmöller, J. J. Clin. Oncol. (2002) [Pubmed]
  12. In vivo excitation of GABA interneurons in the medial prefrontal cortex through 5-HT3 receptors. Puig, M.V., Santana, N., Celada, P., Mengod, G., Artigas, F. Cereb. Cortex (2004) [Pubmed]
  13. Direct interaction of serotonin type 3 receptor ligands with recombinant and native alpha 9 alpha 10-containing nicotinic cholinergic receptors. Rothlin, C.V., Lioudyno, M.I., Silbering, A.F., Plazas, P.V., Casati, M.E., Katz, E., Guth, P.S., Elgoyhen, A.B. Mol. Pharmacol. (2003) [Pubmed]
  14. Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig. Lankiewicz, S., Lobitz, N., Wetzel, C.H., Rupprecht, R., Gisselmann, G., Hatt, H. Mol. Pharmacol. (1998) [Pubmed]
  15. Prevention of chemotherapy-induced nausea and vomiting by tropisetron (Navoban) alone or in combination with other antiemetic agents. Bruntsch, U., Drechsler, S., Eggert, J., Gosse, H., Ukena, D., Imhoff, W., Faerber, L. Semin. Oncol. (1994) [Pubmed]
  16. Antagonism of serotonin3 (5-HT3) receptors within the blood-brain barrier prevents cisplatin-induced emesis in dogs. Gidda, J.S., Evans, D.C., Cohen, M.L., Wong, D.T., Robertson, D.W., Parli, C.J. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  17. Induction of emesis in Suncus murinus by pyrogallol, a generator of free radicals. Torii, Y., Saito, H., Matsuki, N. Br. J. Pharmacol. (1994) [Pubmed]
  18. Probable involvement of the 5-hydroxytryptamine(4) receptor in methotrexate-induced delayed emesis in dogs. Yamakuni, H., Sawai, H., Maeda, Y., Imazumi, K., Sakuma, H., Matsuo, M., Mutoh, S., Seki, J. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  19. Inhibition of 5-hydroxytryptamine- and enterotoxin-induced fluid secretion by 5-HT receptor antagonists in the rat jejunum. Beubler, E., Schirgi-Degen, A., Gamse, R. Eur. J. Pharmacol. (1993) [Pubmed]
  20. Psychosocial stress-induced hypertension results from in vivo expression of long-term potentiation in rat sympathetic ganglia. Alkadhi, K.A., Alzoubi, K.H., Aleisa, A.M., Tanner, F.L., Nimer, A.S. Neurobiol. Dis. (2005) [Pubmed]
  21. Opposite effects of presynaptic 5-HT3 receptor activation on spontaneous and action potential-evoked GABA release at hippocampal synapses. Dorostkar, M.M., Boehm, S. J. Neurochem. (2007) [Pubmed]
  22. In vitro characterization of cytochrome P450 catalysed metabolism of the antiemetic tropisetron. Firkusny, L., Kroemer, H.K., Eichelbaum, M. Biochem. Pharmacol. (1995) [Pubmed]
  23. Morphine induced changes in ethanol-and water-intake are attenuated by the 5-HT3/4 antagonist tropisetron (ICS 205-930). Hodge, C.W., Niehus, J.S., Samson, H.H. Psychopharmacology (Berl.) (1995) [Pubmed]
  24. The 5-HT3 receptor antagonist tropisetron inhibits T cell activation by targeting the calcineurin pathway. Vega, L.d.e. .L., Muñoz, E., Calzado, M.A., Lieb, K., Candelario-Jalil, E., Gschaidmeir, H., Färber, L., Mueller, W., Stratz, T., Fiebich, B.L. Biochem. Pharmacol. (2005) [Pubmed]
  25. Central serotonin 3 receptors play an important role in the modulation of nociceptive neural activity of trigeminal subnucleus caudalis and nocifensive orofacial behavior in rats with persistent temporomandibular joint inflammation. Okamoto, K., Kimura, A., Donishi, T., Imbe, H., Senba, E., Tamai, Y. Neuroscience (2005) [Pubmed]
  26. Pharmacological characterization of the 5-hydroxytryptamine receptor mediating relaxation in the rat isolated ileum. Tuladhar, B.R., Costall, B., Naylor, R.J. Br. J. Pharmacol. (1996) [Pubmed]
  27. Nicotinic receptors co-localize with 5-HT(3) serotonin receptors on striatal nerve terminals. Nayak, S.V., Rondé, P., Spier, A.D., Lummis, S.C., Nichols, R.A. Neuropharmacology (2000) [Pubmed]
  28. Analysis of cumulative probabilities shows that the efficacy of 5HT3 antagonist prophylaxis is not maintained. de Wit, R., Schmitz, P.I., Verweij, J., de Boer-Dennert, M., de Mulder, P.H., Planting, A.S., van der Burg, M.E., Stoter, G. J. Clin. Oncol. (1996) [Pubmed]
  29. Tropisetron: an update of its use in the prevention of chemotherapy-induced nausea and vomiting. Simpson, K., Spencer, C.M., McClellan, K.J. Drugs (2000) [Pubmed]
  30. Intestinal serotonin acts as a paracrine substance to mediate vagal signal transmission evoked by luminal factors in the rat. Zhu, J.X., Zhu, X.Y., Owyang, C., Li, Y. J. Physiol. (Lond.) (2001) [Pubmed]
  31. Effects of 5HT3 receptor antagonism by tropisetron on the sleep EEG and on nocturnal hormone secretion. Rothe, B., Guldner, J., Hohlfeldt, E., Lauer, C.J., Pollmächer, T., Holsboer, F., Steiger, A. Neuropsychopharmacology (1994) [Pubmed]
  32. Efficacy and tolerability of tropisetron in comparison with a combination of tropisetron and dexamethasone in the control of nausea and vomiting induced by cisplatin-containing chemotherapy. Sorbe, B., Högberg, T., Himmelmann, A., Schmidt, M., Räisänen, I., Stockmeyer, M., de Bruijn, K.M. Eur. J. Cancer (1994) [Pubmed]
  33. The polymorphic cytochrome P-4502D6 is involved in the metabolism of both 5-hydroxytryptamine antagonists, tropisetron and ondansetron. Fischer, V., Vickers, A.E., Heitz, F., Mahadevan, S., Baldeck, J.P., Minery, P., Tynes, R. Drug Metab. Dispos. (1994) [Pubmed]
  34. Antiinflammatory effects of 5-HT3 receptor antagonists in lipopolysaccharide-stimulated primary human monocytes. Fiebich, B.L., Akundi, R.S., Lieb, K., Candelario-Jalil, E., Gmeiner, D., Haus, U., Müller, W., Stratz, T., Muñoz, E. Scand. J. Rheumatol. Suppl. (2004) [Pubmed]
  35. 5-HT2A receptor subtype is involved in the thermal hyperalgesic mechanism of serotonin in the periphery. Tokunaga, A., Saika, M., Senba, E. Pain (1998) [Pubmed]
  36. Contribution of peripheral 5-HT2A or 5-HT3 receptors to Fos expression in the trigeminal spinal nucleus produced by acute injury to the masseter muscle during persistent temporomandibular joint inflammation in rats. Okamoto, K., Kimura, A., Donishi, T., Imbe, H., Nishie, Y., Matsushita, H., Tamai, Y., Senba, E. Neuroscience (2006) [Pubmed]
  37. Optimal combination therapy with tropisetron in 445 patients with incomplete control of chemotherapy-induced nausea and vomiting. Hulstaert, F., Van Belle, S., Bleiberg, H., Canon, J.L., Dewitte, M., Buyse, M., De Keyser, P., Westelinck, K.J. J. Clin. Oncol. (1994) [Pubmed]
  38. Analgesic effect of acetaminophen in humans: first evidence of a central serotonergic mechanism. Pickering, G., Loriot, M.A., Libert, F., Eschalier, A., Beaune, P., Dubray, C. Clin. Pharmacol. Ther. (2006) [Pubmed]
  39. Tropisetron, a new 5-HT3-receptor antagonist, in the prevention of radiation-induced nausea, vomiting and diarrhoea. Sorbe, B., Berglind, A.M. Drugs (1992) [Pubmed]
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